KIM, YONG ZU,金容柱,OH, YEONG SOO,吴英秀,吳英秀,CHAE, JEIWOOK,蔡济旭,蔡濟旭,SONG, HO YOUNG,宋昊永,CHUNG, CHUL-WOONG,郑哲雄,鄭哲雄,PARK, YUN HEE,朴允姬,CHOI, HYO JUNG,崔孝汀,PARK, KYUNG EUN,朴庆恩,朴慶恩,KIM, HYOUNGRAE,金炯
申请号：
TW105138779
公开号：
TW201728340A
申请日:
2016.11.25
申请国别(地区):
TW
年份:
2017
代理人:
摘要：
In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody； a linker； and at least two active agents. In preferred embodiments, the linker comprises a peptide sequence of a plurality of amino acids, and at least two of the active agents are covalently coupled to side chains of the amino acids. The antibody-drug conjugate may comprise a self-immolative group, preferably two-self-immolative groups. The linker may comprise an O-substituted oxime,e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent； and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.在一些態樣中，本發明係關於一種抗體-藥物結合物，其包含抗體；連接子；及至少兩種活性劑。在較佳實施例中，連接子包含具有複數個胺基酸之肽序列，且活性劑中之至少兩者共價偶合於胺基酸之側鏈。抗體-藥物結合物可包含自消耗基團，較佳兩個自消耗基團。連接子可包含O取代之肟，例如其中肟之氧原子經將肟共價連接於活性劑之基團取代；且肟之碳原子經將肟共價連接於抗體之基團取代。
